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A Transition-state Analogue Inhibitor of Human Renin (H.261): Testin vitroand a Comparison with Captopril in the Anaesthetized Baboon

 

作者: Michael Szelke,   Malcolm Tree,   Brenda Leckie,   D Michael Jones,   Butrus Atrash,   Sheila Beattie,   Brian Donovan,   Allan Hallett,   Maria Hughes,   Anthony Lever,   James Morton,   Javier Sueiras-Diaz,  

 

期刊: Journal of Hypertension  (OVID Available online 1985)
卷期: Volume 3, issue 1  

页码: 13-18

 

ISSN:0263-6352

 

年代: 1985

 

出版商: OVID

 

关键词: Renin inhibitor;blood pressure;angiotensin II;captopril;baboon

 

数据来源: OVID

 

摘要:

H.261, a new transition state inhibitor of human renin with an IC50of 6.9 x 10-10M, was given by intravenous infusion to six anaesthetized baboons. The inhibitor was infused first at 0.1 (µmol/kg/h for 15 min, then at 1.0 µmol/kg/h for a further 15 min. After a recovery period of 2 h in which the animals received 5% dextrose, they were infused with captopril, 25 µmol/kg/h for 15 min. At both rates of infusion H.261 markedly and significantly reduced the enzymatic action of renin in plasma, the blood concentration of angiotensin I, the plasma concentration of angiotensin II and mean arterial pressure. All changes reverted towards or to control values in the subsequent control period. Captopril also lowered plasma angiotensin II concentration and mean arterial pressure markedly and significantly but, as expected for an inhibitor of the angiotensin l-converting enzyme, plasma active renin concentration and blood angiotensin I concentration increased. The changes of angiotensin II and arterial pressure were similar with captopril and H.261

 

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